General Information of Drug (ID: DM8ZHP1)

Drug Name
MCI-186 Drug Info
Synonyms
Edarabone; Edaravone; Methylphenylpyrazolone; Monopyrazolone; Norantipyrine; Norphenazone; Phenylmethylpyrazolone; Radicut; Developer Z; Edaravone [INN]; Phenyl methyl pyrazolone; CDS1_000986; CI Developer 1; IN1263; M0687; MCI 186; Edaravone(jan); Radicut (TN); AE-641/00371017; C.I. Developer 1; Edaravone (JAN/INN); (MCI-186); 1-Fenyl-3-methyl-2-pyrazolin-5-on; 1-Fenyl-3-methyl-2-pyrazolin-5-on [Czech]; 1-Phenyl-3-methyl-5-oxo-2-pyrazoline; 1-Phenyl-3-methyl-5-pyrazolone; 1-Phenyl-3-methylpyrazolone; 1-Phenyl-3-methylpyrazolone-5; 2,4-Dihydro-5-methyl-2-phenyl-3H-pyrazol-3-one; 3-METHYL-1-PHENYL-2-PYRAZOLIN-5-ONE; 3-Methyl-1-phenyl-2-pyrazoline-5-one; 3-Methyl-1-phenyl-5-pyrazolone; 3-Methyl-1-phenylpyrazol-5-one; 5-Methyl-2-phenyl-2,4-dihydro-3H-pyrazol-3-one; 5-methyl-2-phenyl-4H-pyrazol-3-one
Indication
Disease Entry ICD 11 Status REF
Amyotrophic lateral sclerosis 8B60.0 Approved [1]
Cross-matching ID
PubChem CID
4021
ChEBI ID
CHEBI:31530
CAS Number
CAS 89-25-8
TTD Drug ID
DM8ZHP1
VARIDT Drug ID
DR00101
INTEDE Drug ID
DR1756
ACDINA Drug ID
D01030

Molecule(s) Related to This Drug


Drug Therapeutic Target (DTT)
DTT Name DTT ID UniProt ID MOA REF
Apoptosis regulator Bcl-2 (BCL-2) TTJGNVC BCL2_HUMAN Regulator (upregulator) [2]

Drug Transporter (DTP)
DTP Name DTP ID UniProt ID Highest Status REF
Organic anion transporter 1 (SLC22A6) DTQ23VB S22A6_HUMAN Approved [3]
Organic anion transporter 3 (SLC22A8) DTVP67E S22A8_HUMAN Approved [3]

Drug-Metabolizing Enzyme (DME)
DME Name DME ID UniProt ID Highest Status REF
UDP-glucuronosyltransferase 1A1 (UGT1A1) DEYGVN4 UD11_HUMAN Approved [4]

The Expression Level of Molecule(s) in Normal Tissue of Major ADME-Related Organs

Molecule Molecule Type Gene Name Liver Colon Kidney Small Intestine
Apoptosis regulator Bcl-2 (BCL-2) DTT BCL2 3.963 4.739 4.146 4.878
Organic anion transporter 3 (SLC22A8) DTP OAT3 2.722 2.07 8.103 3.597
Organic anion transporter 1 (SLC22A6) DTP OAT1 4.413 2.233 7.194 4.655
Molecule Expression Atlas in Normal Tissue of Major ADME-related organs

The Expression Level of Molecule(s) between Disease Section and Healthy Individual Tissue

The Studied Disease Amyotrophic lateral sclerosis
ICD Disease Classification 8B60.0
Molecule Name Molecule Type Gene Name p-value Fold-Change Z-score
Apoptosis regulator Bcl-2 (BCL-2) DTT BCL2 2.52E-02 0.17 0.72
Organic anion transporter 3 (SLC22A8) DTP OAT3 8.95E-02 -1.21E-01 -4.10E-01
Organic anion transporter 3 (SLC22A8) DTP OAT3 5.50E-01 4.15E-02 1.96E-01
Organic anion transporter 1 (SLC22A6) DTP OAT1 5.80E-01 4.39E-02 1.78E-01
Organic anion transporter 1 (SLC22A6) DTP OAT1 4.64E-01 -3.69E-02 -2.34E-01
UDP-glucuronosyltransferase 1A1 (UGT1A1) DME UGT1A1 6.40E-01 3.70E-02 1.48E-01
UDP-glucuronosyltransferase 1A1 (UGT1A1) DME UGT1A1 5.01E-01 1.93E-01 4.52E-01
Molecular Expression Atlas between Disease Section and Healthy Individual Tissue

References

1 2017 FDA drug approvals.Nat Rev Drug Discov. 2018 Feb;17(2):81-85.
2 Emerging disease-modifying therapies for the treatment of motor neuron disease/amyotropic lateral sclerosis. Expert Opin Emerg Drugs. 2007 May;12(2):229-52.
3 Human organic anion transporters 1 (hOAT1/SLC22A6) and 3 (hOAT3/SLC22A8) transport edaravone (MCI-186; 3-methyl-1-phenyl-2-pyrazolin-5-one) and its sulfate conjugate. Drug Metab Dispos. 2007 Aug;35(8):1429-34.
4 A novel administration route for edaravone: I. Effects of metabolic inhibitors on skin permeability of edaravone. Int J Pharm. 2009 May 8;372(1-2):33-8.